<br>温度响应性水凝胶罗哌卡因缓释剂在大鼠体内的群体药代动力学分析,Clinical and Experimental Pharmacology and Physiology

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温度响应性水凝胶罗哌卡因缓释剂在大鼠体内的群体药代动力学分析
Clinical and Experimental Pharmacology and Physiology ( IF 2.4 ) Pub Date : 2021-03-08 , DOI: 10.1111/1440-1681.13492
Ji-Yeon Bang ₁ , Sugeun Nam ₁ , Chang-Soon Hwang ₂ , Eun-Kyung Lee ₃ , Byung-Moon Choi ₁

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半衰期短的治疗药物需要频繁给药才能达到持续有效的浓度。这可以使用持续药物输送技术来实现。 PF-72（TGel Bio, Inc.，首尔，韩国）是一种基于从逆热水凝胶冻干获得的粉末的药物输送系统，如果与麻醉剂混合并注射到切口中，可以帮助实现长时间缓解疼痛手术后的部位。对与使用该水凝胶递送的局麻药罗哌卡因的吸收相关的药代动力学参数进行了定量。将10只大鼠分为两组（每组5只），将不同制剂等剂量（4 mg/kg）皮下注射到腹部。实验组接受 PF-72 与 0.75% 罗哌卡因混合，对照组接受 0.75% 罗哌卡因。在特定时间采集血液以测量罗哌卡因的血浆浓度。使用 NOMMEM VII 4 级（ICON Development Solutions，都柏林，爱尔兰）进行群体药代动力学分析。采用结合零级吸收和一级吸收的单室吸收模型来描述罗哌卡因血浆浓度随时间的变化。制剂类型是零级吸收持续时间的显着协变量（实验组，92.9 分钟；对照组，60.5 分钟）。在 0.75% 罗哌卡因中添加 PF-72 增加了吸收到血液中的持续时间，表明注射到手术伤口中的镇痛药的效果更持久。

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Population pharmacokinetic analysis of ropivacaine extended‐release from a temperature‐responsive hydrogel in rats

Therapeutic agents with a short half‐life need to be administered frequently to achieve sustained and effective concentrations. This could be accomplished using sustained drug delivery technology. PF‐72 (TGel Bio, Inc., Seoul, Korea) is a drug delivery system based on a powder obtained from lyophilisation of a reverse thermal hydrogel, which could assist in achieving prolonged pain relief if mixed with an anaesthetic and injected into the incision site following surgery. The pharmacokinetic parameters related to the absorption of the local anaesthetic ropivacaine delivered using this hydrogel were quantified. Ten rats were divided into two groups (n = 5 each), and equal doses (4 mg/kg) of different formulations were subcutaneously injected into the abdomen. The experimental group received PF‐72 mixed with 0.75% ropivacaine, and the control group received 0.75% ropivacaine. Blood was collected at specific times to measure the plasma concentration of ropivacaine. Population pharmacokinetic analysis was performed using NONMEM VII level 4 (ICON Development Solutions, Dublin, Ireland). The one‐compartment absorption model, which combines zero‐order absorption and first‐order absorption, was used to describe the change in ropivacaine plasma concentration over time. The type of formulation was a significant covariate for zero‐order absorption duration (experimental group, 92.9 min; control group, 60.5 min). The addition of PF‐72 to 0.75% ropivacaine increased the duration of absorption into the blood, suggesting a longer lasting effect of the analgesic injected into the surgical wound.

更新日期：2021-05-10

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